As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 847729-27-5, name is Methyl 2-chloro-5-fluoronicotinate, molecular formula is C7H5ClFNO2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. Safety of Methyl 2-chloro-5-fluoronicotinate
[0583] A solution of methyl 2-chloro-5-fluoronicotinate (100 mg, 0.53 mmol) in anhydrous THF (4 mL) was cooled to 0 C and treated with sodium borohydride (120 mg, 3.17 mmol) in a portion-wise manner over a period of 5 min, and the resulting mixture was heated at 70 C for 15 min. Methanol (0.8 mL) was then added in a dropwise manner over 15 min, resulting in considerable effervescence, and the resulting mixture was heated at 70 C for 30 min. The mixture was cooled to ambient temperature and treated with a saturated solution of aqueous ammonium chloride (5 mL). Ethyl acetate (5 mL) was added, resulting in a biphasic mixture, which stirred for 30 min. The organic phase was collected and the aqueous layer was extracted with ethyl acetate (2 x 5 mL). The combined organic phases were then dried over Na2SC>4, filtered and concentrated under vacuum to give the desired product as an orange glass (84 mg, 99%). UPLC-MS (Acidic Method, 2 min): rt = 0.73 min, m/z 162.0/164.0 [M+H]+. ‘H NMR (400 MHz, CDCb) d ppm 8.1 7 (d,.7=3.0 Hz, 1H), 7.71 (ddt, =8.3, 3.0, 0.9, 0.9 Hz, 1H), 4.78 (s, 2H).
With the rapid development of chemical substances, we look forward to future research findings about 847729-27-5.
Reference:
Patent; NFLECTION THERAPEUTICS, INC.; TSAI, Kenneth, Y.; KINCAID, John; SARIN, Kavita, Yang; (319 pag.)WO2020/106303; (2020); A1;,
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